Study on the Influencing Factors of Hypoglycemic Effect of Folate Targeted Polymersomes Encapsulating Insulin

• Published in: Journal of pharmaceutical sciences Vol. 110; no. 5; pp. 2105 - 2113
• Main Authors: Chen, Dao Ge, Zhao, Cheng Wu, Gong, Yan Chun, Li, Zi Ling, Li, Yu Ping, Xiong, Xiang Yuan
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.05.2021
• Subjects: Oral insulin delivery; Polymersomes; TPGS; FA; Polymersomes; Oral insulin delivery; TPGS
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1016/j.xphs.2020.11.042

To study the effects of the density of folic acid (FA) on the hypoglycemic ability of FA-targeted polymersomes as oral insulin carriers. Also to study the change of the hypoglycemic effect of FA-targeted mixed polymersomes added with various mass ratio of d-α-tocopherol polyethylene glycol 1000 succinate (TPGS). The FA-targeted polymersomes with different FA molar contents were prepared. The in vitro insulin release experiments in different media for FA-targeted polymersomes with various FA contents were studied. Their quantitative cellular uptake in Caco-2 cells was examined. The in vivo hypoglycemic activity of FA-targeted polymersomes was also studied with diabetic rats. The polymersomes with the optimal FA molar content was chosen to prepare mixed polymersomes with various TPGS contents. Among insulin-loaded FA-targeted polymersomes with four different FA molar contents, insulin-loaded polymersomes with 10% FA molar content (insulin-loaded 10%FA-Ps) showed the hightest cellular uptake and the best hypoglycemic response. In addition, the insulin-loaded FA-Ps/TPGS5:1 mixed polymersomes exhibited higher cellular uptake and better hypoglycemic response than the other two insulin-loaded mixed polymersomes adding TPGS did. FA-Ps/TPGS5:1 could be a promising formulation for the oral administration of insulin.